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Lurbinectedin

Catalog No. T15793   CAS 497871-47-3
Synonyms: PM01183

Lurbinectedin (PM01183) is a DNA minor groove covalent binder. Lurbinectedin also shows effective anti-tumor activity.

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Lurbinectedin Chemical Structure
Lurbinectedin, CAS 497871-47-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 1,480.00
2 mg In stock $ 1,990.00
5 mg In stock $ 2,960.00
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Purity: 98.11%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lurbinectedin (PM01183) is a DNA minor groove covalent binder. Lurbinectedin also shows effective anti-tumor activity.
Targets&IC50 RMG2:1.16 nM, RMG1:1.25 nM
In vitro Lurbinectedin inhibits RMG1 and RMG2 cell growth (IC50: 1.25 and 1.16 nM, respectively). Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant human ovarian clear cell carcinoma (CCC) cells in vitro[1]. Lurbinectedin-DNA adducts in living cells give rise to double-strand breaks, triggering S-phase accumulation, and apoptosis. Lurbinectedin is a new synthetic tetrahydroisoquinoline alkaloid that is currently in phase I clinical development for the treatment of solid tumors. The potent cytotoxic activity of Lurbinectedin is ascertained in a 23-cell line panel with a mean GI50 value of 2.7 nM[2].
In vivo Lurbinectedin inhibits tumor growth significantly with no weight loss of treated animals, in four murine xenograft models of human cancer[2]. Mouse CCC cell xenografts show that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 causes a significant synergistic effect[1].
Synonyms PM01183
Molecular Weight 784.87
Formula C41H44N4O10S
CAS No. 497871-47-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 15 mg/mL (19.11 mM)

TargetMolReferences and Literature

1. Takahashi R, et al. Preclinical Investigations of PM01183 (Lurbinectedin) as a Single Agent or in Combination with Other Anticancer Agents for Clear Cell Carcinoma of the Ovary. PLoS One. 2016 Mar 17;11(3):e0151050. 2. Leal JF, et al. PM01183, a new DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Br J Pharmacol. 2010 Nov;161(5):1099-110. 3. Vidal A, et al. Lurbinectedin (PM01183), a new DNA minor groove binder, inhibits growth of orthotopic primary graft of NSC 119875-resistant epithelial ovarian cancer. Clin Cancer Res. 2012 Oct 1;18(19):5399-411.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library

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Keywords

Lurbinectedin 497871-47-3 Others DNA/RNA Synthesis inhibit PM-01183 DNA Alkylator/Crosslinker Inhibitor PM01183 PM 01183 inhibitor

 

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